APG-1387

CAS No. 1570231-89-8

APG-1387( —— )

Catalog No. M21856 CAS No. 1570231-89-8

APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    APG-1387
  • Note
    Research use only, not for human use.
  • Brief Description
    APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP).
  • Description
    APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). APG-1387 induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. APG-1387 can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.
  • In Vitro
    Dasminapant (0.02-20 μM; 24 h) induces rapid degradation of cIAPs in HepG2 and HCCLM3 cells.Dasminapant (2 μM; 24 h) enhances TNF-α- and TRAIL-mediated anti-cancer activities in HepG2 and HCCLM3 cells. Dasminapant sensitizes HepG2 and HCCLM3 cells to NK cell-mediated killing in vitro. Western Blot AnalysisCell Line:HepG2 and HCCLM3 cellsConcentration:0.02, 0.2, 2, 20 μM Incubation Time:1, 6, 24 hours Result:Decreased the expression of cIAP1 and cIAP2 in both cell lines in a dose- and time-dependent manner.Inhibited the expression of X chromosome-linked IAP (XIAP) at a high dose.
  • In Vivo
    Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) sensitizes HCCLM3 tumors toward NK cell-mediated killing in mice.Dasminapant (20 mg/kg; i.p. every 3 days for 4 weeks) monotherapy exhibits some degree of anti-tumor effect and is well tolerated in mice. Animal Model:Non-obese diabetic and severe combined immunodeficiency (NOD-SCID) mice bearing HCCLM3 tumors are injected with NK cells Dosage:20 mg/kg Administration:I.p. every 3 days for 4 weeks Result:Decreased the expression of cIAP1 and cIAP2, and less potent to XIAP expression.Potentiated the effects of pre-activated NK cells on HCCLM3 xenograft tumor growth and tumor weight.
  • Synonyms
    ——
  • Pathway
    Apoptosis
  • Target
    IAP
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1570231-89-8
  • Formula Weight
    1157.4
  • Molecular Formula
    C??H??N??O??S?
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 50 mg/mL (43.20 mM; Need ultrasonic)
  • SMILES
    O=S(C1=CC=CC(S(=O)(N(C[C@@H]2NC([C@@H](NC)C)=O)CC[C@](CC[C@H]3C(NC(C4=CC=CC=C4)C5=CC=CC=C5)=O)([H])N3C2=O)=O)=C1)(N(C[C@@H]6NC([C@@H](NC)C)=O)CC[C@](CC[C@H]7C(NC(C8=CC=CC=C8)C9=CC=CC=C9)=O)([H])N7C6=O)=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Chen Z, et, al. The SMAC Mimetic APG-1387 Sensitizes Immune-Mediated Cell Apoptosis in Hepatocellular Carcinoma. Front Pharmacol. 2018 Nov 6; 9:1298. 2. Li BX, et, al. Novel smac mimetic APG-1387 elicits ovarian cancer cell killing through TNF-alpha, Ripoptosome and autophagy mediated cell death pathway. J Exp Clin Cancer Res. 2018 Mar 12;37(1):53. 3. Li N, et, al. A novel Smac mimetic APG-1387 demonstrates potent antitumor activity in nasopharyngeal carcinoma cells by inducing apoptosis. Cancer Lett. 2016 Oct 10;381(1):14-22.
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